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ARV-110

CAS No. : 2222112-77-6

MCE 站：ARV-110

产品活性：ARV-110 是一种具有口服活性的，特异性的雄激素受体 (AR) PROTAC 类降解剂。ARV-110 能促进 AR 的泛素化和降解，可用于前列腺癌的研究。

研究领域：Others

作用靶点：Androgen Receptor

In Vitro: ARV-110 completely degrades AR in all cell lines tested, with an observed 50% degradation concentration (DC₅₀) < 1 nM.
ARV-110 (0.01 nM-300 nM) leads to AR degradation in LNCaP cells in a dose-dependent manner.
ARV-110 (10 nM; 0.5-24 hours) leads to AR degradation in VCaP cells in a time-dependent manner.
ARV-110 (10-1000 nM) suppresses the expression of the AR-target gene PSA, inhibits AR-dependent cell proliferation, and induces apoptosis at low nanomolar concentrations.
ARV-110 (0.01 nM-100 nM) degrades clinically relevant mutant AR proteins (WT AR, F876L, T877A, M896V and H874V), and retains activity in a high androgen environment (R1881, 100 nM) in VCaP cells.

In Vivo: ARV-110 (oral gavage; 1 mg/kg; QD) exhibits a greater than 90% AR degradation in vivo. In LNCaP, VCaP and prostate cancer patient derived xenograft (PDX) models, ARV-110 also exhibits significant inhibition of tumor growth and AR signaling.
ARV-110 (oral gavage; 3 or 10 mpk; 30 days) demonstrates in vivo efficacy and reduction of AR-target gene expression in a long term, castrate, enzalutamide-resistant VCaP tumor model. The TGI are 70% and 60% for 3 mpk and 10 mpk dosage. Respectively.

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